1. Epigenetics
  2. DNA Methyltransferase

DNA Methyltransferase

DNA methylation, defined by the addition of a methyl group to adenine or cytosine bases in DNA catalyzed by DNA methyltransferases (MTases), is one of the most studied post-replicative DNA modification mechanism in bacteria. The three forms of nucleotide methylation identified to date are: N6-methyladenine(m6A), N4-methylcytosine (m4C), and 5-methylcytosine (m5C).

DNA methylation, one type of epigenetic modification, represses gene expression. DNA methylation is caused primarily by a family of DNA methyltransferases (DNMTs) including DNMT1, DNMT3a and DNMT3b. Conventionally, DNMT1 acts as the primary maintenance methyltransferase to keep the methylation of DNA that is already established at the genome, whereas DNMT3a and DNMT3b are classified asde novo methyltransferases to reversibly methylate unmethylated DNA. DNA methylation represses gene transcription through several mechanisms including physically blocking the binding of transcription factors and/or functioning as docking sites for transcriptional repressors/corepressors.

In epigenetic transcriptional regulation, which is important for embryonic development, DNA-methylation patterns are determined by de novo methylation by the DNA methyltransferases Dnmt3a and Dnmt3b in the embryo.

DNA methylation on the cytosine of CpGdinucleotides in gene promoter regions is associated with silencing gene expression. Of the DNA methyltransferases, only DNA methyltransferase 3a (DNMT3a) and 3b (DNMT3b) are capable of adding de novo CpG methylation marks and thus may dynamically regulate gene silencing.

DNA Methyltransferase 相关产品 (16):

Cat. No. Product Name Effect Purity
  • HY-10586
    5-Azacytidine Inhibitor 99.97%
    5-Azacytidine 是一种胞苷类似物,通过限制 DNA 甲基转移酶来抑制DNA甲基化。
  • HY-A0004
    Decitabine Inhibitor 99.99%
    Decitabine 是一种胞嘧啶类似物,为 DNA methyltransferase 抑制剂。
  • HY-13653
    (-)-Epigallocatechin Gallate Inhibitor 99.60%
    (-)-Epigallocatechin Gallate 是一种天然的多酚黄酮类化合物,能够抑制 telomeraseDNA methyltransferase 的活性,同时阻止 EGF 受体和 HER-2 受体活化。
  • HY-13962
    SGI-1027 Inhibitor 99.77%
    SGI-1027是DNA甲基转移酶(DNMT)抑制剂,对DNMT1,DNMT3A和DNMT3B的IC50分别为6,8和7.5 μM。
  • HY-13642
    RG108 Inhibitor 99.75%
    RG108 是一种非核苷的 DNA 甲基转移酶 (DNA methyltransferase) 抑制剂,IC50 值为 115 nM。
  • HY-13542
    SGI-110 Inhibitor
    SGI-110 是 DNA 甲基转移酶 (DNMT) 的抑制剂。
  • HY-B2194
    γ-Oryzanol Inhibitor
    γ-Oryzanol 有效抑制小鼠纹状体中的 DNA 甲基转移酶 (DNMTs)。 抑制 DNMT1DNMT3aIC50 分别为 3.2 μM 和 22.3 μM。
  • HY-13420
    Zebularine Inhibitor >98.0%
    Zebularine (NSC309132; 4-Deoxyuridine)是DNA甲基转移酶抑制剂;也是胞苷脱氨酶抑制剂,Ki值为0.95 μM。
  • HY-N0141
    Parthenolide Inhibitor 99.13%
    Parthenolide 是一种 NF-κB 抑制剂,可降低组蛋白脱乙酰酶 1 (HDAC-1) 和 DNA 甲基转移酶 1。
  • HY-13765
    6-Thioguanine Inhibitor 99.94%
  • HY-13668
    Lomeguatrib Inhibitor
    Lomeguatrib (PaTrin-2)是高活性O6-alkylguanine-DNA alkyltransferase(MGMT)抑制剂,IC50为6 nM。
  • HY-12747
    DC_517 Inhibitor >98.0%
    DC_517是一种新型的, 选择性, 非核苷类的 DNA甲基转移酶1 (DNMT1) 抑制剂 (IC50 = 1.7 μM)。
  • HY-B2230
    Hinokitiol Inhibitor >98.0%
    Hinokitiol 是从日本扁柏中分离到的挥发油成分,具有抗感染、抗氧化及抗肿瘤等活性。
  • HY-B1109
    N-Acetylprocainamide Inhibitor 99.90%
    N-Acetylprocainamide是Procainamide的N-乙酰化的代谢物。这是一个Ⅲ类抗心律失常药物, 而Procainamide是Ia类抗心律失常药物。
  • HY-12746
    DC_05 Inhibitor
  • HY-13057
    Glucose-conjugated MGMT inhibitor Inhibitor
    O6BTG-C8-βGlu是葡萄糖耦合的MGMT抑制剂,IC50为32 nM,对HeLa S3的IC50为10 nM。